ChEMBL ligand: CHEMBL5095223 (AZD-9574, AZD9574, PALACAPARIB, Azd-9574)
poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase 1 in Human [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874] There should be some charts here, you may need to enable JavaScript!
poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
poly(ADP-ribose) polymerase 1/Poly [ADP-ribose] polymerase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3105] [GtoPdb: 2771] [UniProtKB: P09874]
ChEMBL	Binding affinity to CM5 chip-immobilized GST-tagged PARP1 (unknown origin) assessed as dissociation constant by SPR analysis	B	9.27	pKd	0.54	nM	Kd	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]
ChEMBL	Inhibition of PARP1 (unknown origin) measured after 2 hrs by ELISA	B	6.06	pIC50	870	nM	IC50	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]
ChEMBL	Inhibition of PARP1 in wild type human A549 cells preincubated with compound for 1 hr followed by H2O2 addition and measured after 5 mins by PARylation inhibition assay	B	7.71	pIC50	19.5	nM	IC50	J Med Chem (2025) 68: 1731-1754 [PMID:39789975]
GtoPdb	-	-	8.3	pIC50	<5	nM	IC50	WO2021260092A1. Quinoxaline derivatives as anti-cancer drugs (2021)
ChEMBL	Inhibition of PARP1 (unknown origin) expressed in Escherichia coli BL21 incubated for 60 mins	B	8.3	pIC50	<5	nM	IC50	J Med Chem (2024) 67: 11488-11521 [PMID:38955347]
ChEMBL	Inhibition of N-terminal 6His-tagged full-length recombinant human PARP1 by fluorescence anisotropy assay	B	8.3	pIC50	<5	nM	IC50	J Med Chem (2024) 67: 21717-21728 [PMID:39655996]
ChEMBL	Inhibition of PARP1 in PARP2 knockout human A549 cells preincubated with compound for 1 hr followed by H2O2 addition and measured after 5 mins by selective targeting PARylation inhibition assay	B	8.74	pIC50	1.8	nM	IC50	J Med Chem (2025) 68: 1731-1754 [PMID:39789975]
ChEMBL	Inhibition of PARP1 (unknown origin) assessed as increase in DNA trapping activity measured after 180 mins by fluorescence anisotropy binding assay	B	6.53	pEC50	296.6	nM	EC50	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]
ChEMBL	Inhibition of PARP1 (unknown origin) assessed as increase in DNA trapping activity measured after 120 mins by fluorescence anisotropy binding assay	B	6.81	pEC50	153.4	nM	EC50	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]
ChEMBL	Inhibition of PARP1 (unknown origin) assessed as increase in DNA trapping activity measured after 60 mins by fluorescence anisotropy binding assay	B	7.52	pEC50	30.1	nM	EC50	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]
poly(ADP-ribose) polymerase 2/Poly [ADP-ribose] polymerase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5366] [GtoPdb: 2772] [UniProtKB: Q9UGN5]
GtoPdb	-	-	4.03	pIC50	93000	nM	IC50	WO2021260092A1. Quinoxaline derivatives as anti-cancer drugs (2021)
ChEMBL	Inhibition of N-terminal 6His-tagged full-length recombinant human PARP2 by fluorescence anisotropy assay	B	4.03	pIC50	>93000	nM	IC50	J Med Chem (2024) 67: 21717-21728 [PMID:39655996]
ChEMBL	Inhibition of PARP2 in PARP1 knockout human A549 cells preincubated with compound for 1 hr followed by H2O2 addition and measured after 5 mins by selective targeting PARylation inhibition assay	B	6	pIC50	>1000	nM	IC50	J Med Chem (2025) 68: 1731-1754 [PMID:39789975]
ChEMBL	Inhibition of N-terminal GST-tagged human PARP2 (2 to 583 residues) expressed in baculovirus infected Sf9 cells assessed as increase in DNA trapping activity measured after 60 mins by fluorescence anisotropy binding assay	B	5.14	pEC50	7263	nM	EC50	J Med Chem (2024) 67: 21380-21399 [PMID:39571073]

ChEMBL data shown on this page come from version 37:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]